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Identification of a sulfonamide series of CCR2 antagonists |
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| Authors: | Simon Peace Joanne Philp Carl Brooks Val Piercy Kitty Moores Chris Smethurst Steve Watson Simon Gaines Mara Zippoli Claudette Mookherjee Robert Ife |
| Affiliation: | 1. GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK;2. GlaxoSmithKline, Upper Merion, 709 Swedeland Road, King of Prussia, PA 19406, USA;3. GlaxoSmithKline, New Frontiers Science Park, Harlow CM19 5MW, UK |
| Abstract: | A series of sulfonamide CCR2 antagonists was identified by high-throughput screening. Management of molecular weight and physical properties, in particular moderation of lipophilicity and study of pKa, yielded highly potent CCR2 antagonists exhibiting good pharmacokinetic properties and improved potency in the presence of human plasma. |
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